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1. 发明授权

US5534532A Aliphatic amino bis-aryl squalene synthase inhibitors 失效
公开(公告)号：US5534532A
公开(公告)日：1996-07-09
申请号：US378146
申请日：1995-01-25
申请人： Robert A. Groneberg , John R. Regan , Kent W. Neuenschwander , Anthony C. Scotese
发明人： Robert A. Groneberg , John R. Regan , Kent W. Neuenschwander , Anthony C. Scotese
IPC分类号： C07C217/22 , C07C233/75 , C07C235/56 , C07D263/56 , C07D263/57 , C07D413/12 , A61K31/425 , C07D277/64 , C07D277/66
CPC分类号： C07D263/57 , C07C217/22 , C07C233/75 , C07C235/56 , C07D413/12
摘要： This invention relates to a class of novel aliphatic amino bis-aryl compounds containing at least four carbon atoms and an amino group either substituted thereon or incorporated therein and is further linked or bridged to two mono- and/or bicyclic rings. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.

2. 发明授权

US5455260A Aliphatic amino bis-aryl squalene synthase inhibitors 失效
标题翻译：脂肪族氨基双芳基角鲨烯合酶抑制剂
公开(公告)号：US5455260A
公开(公告)日：1995-10-03
申请号：US65966
申请日：1993-05-21
申请人： Robert A. Groneberg , John R. Regan , Kent W. Neuenschwander , Anthony C. Scotese
发明人： Robert A. Groneberg , John R. Regan , Kent W. Neuenschwander , Anthony C. Scotese
IPC分类号： C07C217/22 , C07C233/75 , C07C235/56 , C07D263/56 , C07D263/57 , C07D413/12 , A61K31/42
CPC分类号： C07D263/57 , C07C217/22 , C07C233/75 , C07C235/56 , C07D413/12
摘要： This invention relates to a class of novel aliphatic amino bis-aryl compounds containing at least four carbon atoms and an amino group either substituted thereon or incorporated therein and is further linked or bridged to two mono- and/or bicyclic rings. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.
摘要翻译：本发明涉及一类新的脂族氨基双芳基化合物，其含有至少四个碳原子和在其上取代或并入其中的氨基，并进一步连接或桥连至两个单环和/或双环。本发明化合物降低体内血清胆固醇水平，而不显着降低甲羟戊酸代谢物合成。本发明还涉及使用本发明化合物降低血清胆固醇水平的药物组合物和治疗方法。

3. 发明授权

US4537968A Thiophene derivatives with antisecretory activity 失效
标题翻译：具有抗分泌活性的噻吩衍生物
公开(公告)号：US4537968A
公开(公告)日：1985-08-27
申请号：US564440
申请日：1983-12-21
申请人： Anthony C. Scotese , Robert L. Morris , Arthur A. Santilli , Donald P. Strike
发明人： Anthony C. Scotese , Robert L. Morris , Arthur A. Santilli , Donald P. Strike
IPC分类号： C07D333/38 , C07D333/42 , C07D417/12 , C07D413/12 , C07D333/36
CPC分类号： C07D417/12 , C07D333/38 , C07D333/42
摘要： Compounds of the formula: ##STR1## wherein A is ##STR2## R is mono- or dihalo, amino, nitro, cyano, hydroxy, trifluoromethyl, mercapto, lower alkyl, lower alkoxy, alkanoyl, lower cycloalkyl, carboxy, alkoxycarbonyl, mono- or di-lower alkyl substituted amino, alkanoylamino, lower alkyl thio, loweralkyl-sulfonyl, sulfamoyl, lower alkyl substituted sulfamoyl, phenyl or phenyl substituted with halo, lower alkyl, lower alkoxy, trifluoromethyl, hydroxy, amino, cyano or nitro;X and Y are each, independently, hydrogen or ##STR3## wherein R.sup.1 is hydrogen or lower alkyl;R.sup.2 is hydrogen or lower alkyl; orR.sup.1 and R.sup.2 taken together form a heterocyclic moiety selected from 1-pyrrolidinyl, 1-piperidinyl, 1-hexahydroazepinyl, 1-octahydroazocinyl, 3-thiazolidinyl, 4-morpholinyl or 4-thiomorpholinyl, with the proviso that one of X and Y is always hydrogen;n is 1-4;and the pharmacologically acceptable salts thereof, which are intermediates in preparing H.sub.2 receptor antagonists and which also have antisecretory/antiulcer activity.
摘要翻译：硝基，氰基，羟基，三氟甲基，巯基，低级烷基，低级烷氧基，烷酰基，低级环烷基，羧基，烷氧基羰基，单 - 或二低级烷基取代的氨基，烷酰基氨基，低级烷基硫代，低级烷基 - 磺酰基，氨磺酰基，低级烷基取代的氨磺酰基，苯基或被卤素，低级烷基，低级烷氧基，三氟甲基，羟基，氨基，氰基或硝基取代的苯基。 X和Y各自独立地为氢或者其中R 1为氢或低级烷基; R2是氢或低级烷基; 或者R 1和R 2一起形成选自1-吡咯烷基，1-哌啶基，1-六氢氮杂基，1-八氢吖嗪基，3-噻唑烷基，4-吗啉基或4-硫代吗啉基的杂环部分，条件是X和Y之一为总是氢; n为1-4; 和其药理学上可接受的盐，它们是制备H 2受体拮抗剂的中间体，并且也具有抗分泌/抗溃疡活性。

4. 发明授权

US4215123A Antisecretory 4-oxy-3-carboxy or cyano-1,2-dihydro-2-oxo-1,8-naphthyridine derivatives 失效
标题翻译：苯基-4-氧基-3-羧基或氰基-1,2-二氢-2-氧代-1,8-萘啶衍生物
公开(公告)号：US4215123A
公开(公告)日：1980-07-29
申请号：US36921
申请日：1979-05-07
申请人： Anthony C. Scotese , Arthur A. Santilli
发明人： Anthony C. Scotese , Arthur A. Santilli
IPC分类号： C07D213/80 , C07D471/04 , C07D491/04 , A61K31/435
CPC分类号： C07D213/80 , C07D471/04 , C07D491/04
摘要： Substituted 4-oxy-3-carboxy or cyano-1,2-dihydro-2-oxo-1,8-naphthyridine derivatives as gastric antisecretory agents for use in the treatment of peptic ulcer disease.
摘要翻译：取代的4-氧-3-羧基或氰基-1,2-二氢-2-氧代-1,8-萘啶衍生物作为胃溃疡剂用于治疗消化性溃疡病。

5. 发明申请

US20100249101A1 MALONAMIDE DERIVATIVES WITH ANTITHROMBOTIC ACTIVITY 有权
标题翻译：具有抗血栓活性的马来酰胺衍生物
公开(公告)号：US20100249101A1
公开(公告)日：2010-09-30
申请号：US12683736
申请日：2010-01-07
申请人： Henning STEINHAGEN , Hauke SZILLAT , Markus FOLLMANN , Reinhard KIRSCH , Volkmar WEHNER , Hans MATTER , Martin LORENZ , Kent W. Neuenschwander , Anthony C. SCOTESE
发明人： Henning STEINHAGEN , Hauke SZILLAT , Markus FOLLMANN , Reinhard KIRSCH , Volkmar WEHNER , Hans MATTER , Martin LORENZ , Kent W. Neuenschwander , Anthony C. SCOTESE
IPC分类号： A61K31/553 , C07D213/90 , A61K31/455 , C07C237/20 , A61K31/167 , A61K31/4409 , C07D265/30 , A61K31/5375 , C07D309/08 , A61K31/351 , C07D211/66 , A61K31/4465 , C07D211/42 , C07D409/12 , A61K31/381 , C07D207/12 , A61K31/4015 , C07D277/24 , A61K31/426 , C07D241/04 , A61K31/4965 , C07D241/18 , C07D267/10 , A61P9/00 , A61P11/00 , A61P31/12 , A61P35/00 , A61P29/00
CPC分类号： C07D213/80 , C07C257/18 , C07C311/08 , C07C311/46 , C07C317/22 , C07C317/32 , C07C2601/14 , C07D211/42 , C07D213/30 , C07D213/34 , C07D309/08 , C07D409/12 , C07D413/12
摘要： The present invention relates to compounds of formula I, The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are inhibitors of the blood clotting enzymes, especially factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
摘要翻译：本发明涉及式I化合物。式I化合物是有价值的药理学活性化合物。它们表现出强烈的抗血栓形成作用，并且适用于治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。它们是血液凝固酶，特别是因子VIIa的抑制剂，并且通常可用于其中存在不需要的因子VIIa的活性或用于治疗或预防因子VIIa的抑制的条件。本发明还涉及制备式I化合物的方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物制剂。

6. 发明授权

US5494918A Multicyclic tertiary amine polyaromatic squalene syntase inhibitors 失效
标题翻译：多元叔胺多芳族角鲨烯合成酶抑制剂
公开(公告)号：US5494918A
公开(公告)日：1996-02-27
申请号：US320075
申请日：1994-10-07
申请人： Kent Neuenschwander , Dilip Amin , Anthony C. Scotese , Robert L. Morris
发明人： Kent Neuenschwander , Dilip Amin , Anthony C. Scotese , Robert L. Morris
IPC分类号： A61K31/435 , A61K31/44 , A61K31/505 , A61P3/06 , A61P43/00 , C07D221/22 , C07D223/02 , C07D223/14 , C07D239/06 , C07D453/02 , C07D455/00 , C07D471/08 , C07D471/18 , C07D495/08 , C07D519/00 , C12N9/99
CPC分类号： C07D453/02
摘要： This invention relates to polycyclic compounds containing two mono- and/or bicyclic rings and a basic tertiary amino group capable of forming an ammonium ion at biological pH and which reduces levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.
摘要翻译：本发明涉及含有两个单环和/或二环的多环化合物和能够在生物pH下形成铵离子的碱性叔氨基，并且能降低体内血清胆固醇水平而不显着降低甲羟戊酸代谢物合成。本发明还涉及使用本发明化合物降低血清胆固醇水平的药物组合物和治疗方法。

7. 发明授权

US5395846A Amino Bi- and tri-carbocyclic aklane bis-aryl squalene synthase inhibitors 失效
标题翻译：氨基双 - 和三 - 碳环烷基双芳基角鲨烯合酶抑制剂
公开(公告)号：US5395846A
公开(公告)日：1995-03-07
申请号：US83117
申请日：1993-06-25
申请人： Robert L. Morris , Kent W. Neuenschwander , Keith S. Learn , Anthony C. Scotese
发明人： Robert L. Morris , Kent W. Neuenschwander , Keith S. Learn , Anthony C. Scotese
IPC分类号： C07D263/56 , C07D263/57 , A61K31/42
CPC分类号： C07D263/57
摘要： This invention relates to a class of novel amino bi- and tri-carbocyclic alkane compounds having bis-aryl substitution which exhibit squalene synthase inhibition properties. The bi- and tri-carbocyclic alkane ring contains an amino group and the ring is further linked or bridged to two mono- and/or bicyclic rings. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.
摘要翻译：本发明涉及一类具有双芳基取代的新型氨基双 - 和三 - 碳环烷烃化合物，其表现出角鲨烯合酶抑制性质。双 - 和三 - 碳环烷烃环包含一个氨基，并且该环进一步连接或桥连至两个单环和/或双环。本发明化合物降低体内血清胆固醇水平，而不显着降低甲羟戊酸代谢物合成。本发明还涉及使用本发明化合物降低血清胆固醇水平的药物组合物和治疗方法。

8. 发明授权

US5081253A Imidazo(4,5-C)pyridines as antiosteoporotic agents 失效
标题翻译：咪唑（4,5-C）吡啶类作为抗菌药
公开(公告)号：US5081253A
公开(公告)日：1992-01-14
申请号：US557247
申请日：1990-07-24
申请人： Arthur A. Santilli , Anthony C. Scotese , Donald P. Strike
发明人： Arthur A. Santilli , Anthony C. Scotese , Donald P. Strike
IPC分类号： A61K31/435 , A61P3/02 , A61P43/00 , C07D471/04
CPC分类号： C07D471/04
摘要： This invention relates to 2-substituted-imidazo[4,5-c]pyridines, to the process for their preparation, to pharmaceutical compositions containing said 2-substituted-imidazo[4,5-c]pyridines and to the use of said 2-substituted-imidazo[4,5-c]pyridines for modifying the balance between bone production and bone resorption in a host animal, including man.

9. 发明授权

US4904691A Novel HMG-CoA reductase inhibitors 失效
标题翻译：新型HMG-CoA还原酶抑制剂
公开(公告)号：US4904691A
公开(公告)日：1990-02-27
申请号：US321950
申请日：1989-03-10
申请人： Kent W. Neuenschwander , Anthony C. Scotese
发明人： Kent W. Neuenschwander , Anthony C. Scotese
IPC分类号： A61K31/365 , C07C59/54 , C07C59/56 , C07C59/64 , C07C69/732 , C07C69/738 , C07D309/30 , C07D405/04
CPC分类号： C07C59/54 , C07C59/56 , C07C59/64 , C07D309/30 , Y10S514/824
摘要： Disclosed are novel 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors useful as antihypercholesterolemic agents represented by the formula ##STR1## and the corresponding ring-opened hydroxy acids and esters derived therefrom and pharmaceutically acceptable salts thereof.Pharmaceutical compositions containing said compounds and method of inhibiting the biosynthesis of cholesterol therewith are also disclosed.
摘要翻译：公开了新型3-羟基-3-甲基戊二酰辅酶A还原酶抑制剂，其用作由式＆lt; IMAGE＆gt;表示的抗高血胆固醇药和相应的开环羟基酸及其衍生的酯及其药学上可接受的盐。还公开了含有所述化合物的药物组合物和抑制胆固醇生物合成的方法。

10. 发明授权

US4621142A Precursors of benzo- and thieno-fused heterocyclic anti-ulcer agents 失效
标题翻译：苯并 - 噻吩并稠合的杂环抗溃疡剂的前体
公开(公告)号：US4621142A
公开(公告)日：1986-11-04
申请号：US760709
申请日：1985-07-30
申请人： Anthony C. Scotese , Arthur A. Santilli , Donald P. Strike
发明人： Anthony C. Scotese , Arthur A. Santilli , Donald P. Strike
IPC分类号： C07D275/06 , C07D513/04 , C07D495/04
CPC分类号： C07D275/06 , C07D513/04
摘要： A process for preparing certain benzo- and thieno-fused heterocyclic compounds having H.sub.2 -receptor antagonist and antisecretory activity, which comprises the amide reduction of N-substituted carbamoyl-containing benzo- or thieno-fused heterocyclic intermediates; and said N-substituted carbamoyl-containing benzo- or thieno-fused heterocyclic intermediates.
摘要翻译：一种制备具有H 2受体拮抗剂和抗分泌活性的某些苯并 - 噻吩并稠合的杂环化合物的方法，其包括N-取代的含氨基甲酰基的苯并或噻吩并稠合的杂环中间体的酰胺还原; 和所述含N-取代氨基甲酰基的苯并或噻吩并稠合的杂环中间体。

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